Details of the PSS

General Information of Protein Scaffold of SBP (PSS) (ID: PS044)
PSS Name	Macrocyclic peptide
Diagrammatic Sketch
Highest Status	Marketed
Class	Non-Antibody
Fold Type	Beta-Sheets + Loops
Sequence Length	`6-23
Molecular Weight	0.5-2 kDa

Parental Protein of This PSS

Parental Protein Name	Synonym		PDB ID	UniProt ID	Origin
Peptide	N.A.		N.A.	N.A.	Synthetic construct

Synthetic Binding Protein (SBP) Featuring this PSS

SBP Name	Highest Status	Template	Expression System	Selection Method	Details	Ref
Macrocyclic peptide Lanreotide	Marketed	N.A.	N.A.	N.A.	SBP Info	[1]
Macrocyclic peptide Octreotide	Marketed	N.A.	N.A.	N.A.	SBP Info	[2]
Macrocyclic peptide Pegcetacoplan	Marketed	N.A.	N.A.	N.A.	SBP Info	[3], [4]
Macrocyclic peptide anti-PCSK9 MK-0616	Phase III	N.A.	N.A.	mRNA display	SBP Info	[5]
Macrocyclic peptide Zilucoplan	Phase III	N.A.	N.A.	N.A.	SBP Info	[6], [7]
Macrocyclic peptide anti-MRP1 CPI1	Research	N.A.	N.A.	N.A.	SBP Info	[8]
Macrocyclic peptide anti-NTS2 CR-01-64	Research	Neurotensin (8-13)	N.A.	N.A.	SBP Info	[9]
Macrocyclic peptide anti-retromer RT-D1	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-D2	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-D3	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-D4	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-L1	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-L2	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-L3	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-retromer RT-L4	Research	N.A.	N.A.	N.A.	SBP Info	[10]
Macrocyclic peptide anti-AKT2 Pakti-L1	Research	N.A.	FIT system	mRNA display	SBP Info	[11]
Macrocyclic peptide anti-AKT2 Pakti-L2	Research	N.A.	FIT system	mRNA display	SBP Info	[11]
Macrocyclic peptide anti-AKT2 Pakti-L3	Research	N.A.	FIT system	mRNA display	SBP Info	[11]
Macrocyclic peptide anti-E6AP CM11-1	Research	N.A.	FIT system	mRNA display	SBP Info	[12]
Macrocyclic peptide anti-E6AP CM11-1S-1	Research	N.A.	FIT system	mRNA display	SBP Info	[12]
Macrocyclic peptide anti-E6AP CM11-3	Research	N.A.	FIT system	mRNA display	SBP Info	[12]
Macrocyclic peptide anti-E6AP CM11-5	Research	N.A.	FIT system	mRNA display	SBP Info	[12]
Macrocyclic peptide anti-EpCAM Epi-1	Research	N.A.	FIT system	mRNA display	SBP Info	[13]
Macrocyclic peptide anti-EpCAM Epi-3	Research	N.A.	FIT system	mRNA display	SBP Info	[13]
Macrocyclic peptide anti-HDAC8 CycH8a	Research	N.A.	Escherichia coli	Phage display	SBP Info	[14]
Macrocyclic peptide anti-SiRT2 S2iD7	Research	N.A.	FIT system	mRNA display	SBP Info	[15]
Macrocyclic peptide anti-SiRT2 S2iL8	Research	N.A.	FIT system	mRNA display	SBP Info	[15]
Macrocyclic peptide anti-TEV-protease CycTev1	Research	N.A.	Escherichia coli	Phage display	SBP Info	[14]
Macrocyclic peptide anti-TEV-protease CycTev2	Research	N.A.	Escherichia coli	Phage display	SBP Info	[14]
Macrocyclic peptide anti-HSA p1	Research	N.A.	N.A.	Transcription-translation coupled with association of PuL display	SBP Info	[16]
Macrocyclic peptide anti-HSA p2	Research	N.A.	N.A.	Transcription-translation coupled with association of PuL display	SBP Info	[16]
Macrocyclic peptide anti-Integrin ALOS4	Research	N.A.	N.A.	Phage display	SBP Info	[17]
Macrocyclic peptide anti-PfMATE MaD8	Research	N.A.	N.A.	Random non-standard peptide integrated discovery system	SBP Info	[18]
Macrocyclic peptide anti-PfMATE MaL6	Research	N.A.	N.A.	Random non-standard peptide integrated discovery system	SBP Info	[18]
Macrocyclic peptide anti-uPA clone 1	Research	N.A.	N.A.	Phage display	SBP Info	[19]
Macrocyclic peptide anti-uPA mupain-1	Research	N.A.	N.A.	Phage display	SBP Info	[19]
Macrocyclic peptide anti-uPA mupain-1-12	Research	Mupain-1	N.A.	N.A.	SBP Info	[19]
Macrocyclic peptide anti-uPA mupain-1-16	Research	Mupain-1	N.A.	N.A.	SBP Info	[19]
Macrocyclic peptide anti-C5 RA-101295	Research	N.A.	N.A.	N.A.	SBP Info	[20]
Macrocyclic peptide anti-C5 RA-101348	Research	N.A.	N.A.	N.A.	SBP Info	[21]
Macrocyclic peptide anti-CmABCB1 aCAP	Research	N.A.	N.A.	N.A.	SBP Info	[22]
Macrocyclic peptide anti-CXCR4 CVX15	Research	N.A.	N.A.	N.A.	SBP Info	[23]
Macrocyclic peptide anti-Integrin P5	Research	N.A.	N.A.	N.A.	SBP Info	[24], [25]
Macrocyclic peptide anti-RANKL OP3-4	Research	N.A.	N.A.	N.A.	SBP Info	[26], [27]

References

1	Patient-Reported Symptom Control of Diarrhea and Flushing in Patients with Neuroendocrine Tumors Treated with Lanreotide Depot/Autogel: Results from a Randomized, Placebo-Controlled, Double-Blind and 32-Week Open-Label Study. Oncologist. 2018 Jan;23(1):16-24.
2	Octreotide and Lanreotide in Gastroenteropancreatic Neuroendocrine Tumors. Curr Oncol Rep. 2016 Jan;18(1):7.
3	C3 inhibition with pegcetacoplan in subjects with paroxysmal nocturnal hemoglobinuria treated with eculizumab. Am J Hematol. 2020 Nov;95(11):1334-1343.
4	Pegcetacoplan versus Eculizumab in Paroxysmal Nocturnal Hemoglobinuria. N Engl J Med. 2021 Mar 18;384(11):1028-1037.
5	Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor. Circulation. 2023 Jul 11;148(2):144-158.
6	ClinicalTrials.gov (NCT04436497) HEALEY ALS Platform Trial - Regimen A Zilucoplan
7	ClinicalTrials.gov (NCT04225871) Open-Label Extension of Zilucoplan in Subjects With Generalized Myasthenia Gravis
8	A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation. Proc Natl Acad Sci U S A. 2023 Mar 14;120(11):e2220012120.
9	Pharmacodynamic and pharmacokinetic profiles of a neurotensin receptor type 2 (NTS2) analgesic macrocyclic analog. Biomed Pharmacother. 2021 Sep;141:111861.
10	De novo macrocyclic peptides for inhibiting, stabilizing, and probing the function of the retromer endosomal trafficking complex. Sci Adv. 2021 Dec 3;7(49):eabg4007.
11	In vitro selection of anti-Akt2 thioether-macrocyclic peptides leading to isoform-selective inhibitors. ACS Chem Biol. 2012 Mar 16;7(3):607-13.
12	Natural product-like macrocyclic N-methyl-peptide inhibitors against a ubiquitin ligase uncovered from a ribosome-expressed de novo library. Chem Biol. 2011 Dec 23;18(12):1562-70.
13	A Fluorescent Imaging Probe Based on a Macrocyclic Scaffold That Binds to Cellular EpCAM. J Mol Evol. 2015 Dec;81(5-6):210-7.
14	A Genetically Encoded, Phage-Displayed Cyclic-Peptide Library. Angew Chem Int Ed Engl. 2019 Oct 28;58(44):15904-15909.
15	Discovery of macrocyclic peptides armed with a mechanism-based warhead: isoform-selective inhibition of human deacetylase SIRT2. Angew Chem Int Ed Engl. 2012 Apr 2;51(14):3423-7.
16	TRAP display: a high-speed selection method for the generation of functional polypeptides. J Am Chem Soc. 2013 Apr 10;135(14):5433-40.
17	Novel synthetic cyclic integrin v3 binding peptide ALOS4: Antitumor activity in mouse melanoma models. Oncotarget. 2016 Sep 27;7(39):63549-63560.
18	A macrocyclic peptide that serves as a cocrystallization ligand and inhibits the function of a MATE family transporter. Molecules. 2013 Aug 30;18(9):10514-30.
19	Structural Principles in the Development of Cyclic Peptidic Enzyme Inhibitors. Int J Biol Sci. 2017 Sep 21;13(10):1222-1233.
20	Inhibition of complement C5 protects against organ failure and reduces mortality in a baboon model of Escherichia coli sepsis. Proc Natl Acad Sci U S A. 2017 Aug 1;114(31):E6390-E6399.
21	Generation of complement molecular complex C5b-9 (C5b-9) in response to poly-traumatic hemorrhagic shock and evaluation of C5 cleavage inhibitors in non-human primates. Int Immunopharmacol. 2018 Jan;54:221-225.
22	Structural basis for gating mechanisms of a eukaryotic P-glycoprotein homolog. Proc Natl Acad Sci U S A. 2014 Mar 18;111(11):4049-54.
23	Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science. 2010 Nov 19;330(6007):1066-71.
24	Crystal structure of the extracellular segment of integrin alpha Vbeta3 in complex with an Arg-Gly-Asp ligand. Science. 2002 Apr 5;296(5565):151-5.
25	N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists. J Med Chem. 1999 Aug 12;42(16):3033-40.
26	The inhibitory effects of a RANKL-binding peptide on articular and periarticular bone loss in a murine model of collagen-induced arthritis: a bone histomorphometric study. Arthritis Res Ther. 2015 Sep 12;17(1):251.
27	Disabling of receptor activator of nuclear factor-kappaB (RANK) receptor complex by novel osteoprotegerin-like peptidomimetics restores bone loss in vivo. J Biol Chem. 2004 Feb 27;279(9):8269-77.